Brar Vivekjot, Kaur Gurpreet
Department of Pharmaceutical Sciences and Drug Research, Punjabi University, Patiala - 147002, Punjab, India.
Pharm Nanotechnol. 2018;6(3):180-191. doi: 10.2174/2211738506666180813122437.
To prepare chitosan-okra gum nanoparticles and their evaluation as mucoadhesive drug delivery system for intranasal delivery of esculin.
Esculin loaded chitosan-okra gum based nanoparticles were prepared using ionic gelation method. The preparation method was optimized using Box-Behnken experimental design employing okra gum concentration, chitosan concentration, pH and stirring speed as independent variables and particle size, encapsulation efficiency and zeta potential of the formulation were selected as dependent variables. The optimized formulation was characterized using FTIR, SEM and TEM. The nanoparticles were evaluated for their bioadhesive strength and in vitro drug release studies. The optimized intranasal formulation was administered to rats and the pharmacokinetic profile and biodistribution studies were carried out to calculate the targeting efficiency of the formulation in the brain.
The nanoparticles were found to depict particle size in the range of 294.0 to 613.4 nm. The concentration of gums was found to significantly influence the particle size and encapsulation efficiency. The nanoparticles depicted bioadhesive strength of 32±2%. The in vitro drug release studies showed 96.4±4.2% release of esculin from nanoparticles in 4h. The drug targeting of NPs to brain was found to be nearly double that of esculin given as simple solution.
The nanoparticles prepared using chitosan-okra gum were found to possess good mucoadhesive strength with and high brain targeting efficiency.
制备壳聚糖-秋葵胶纳米粒，并评估其作为载有七叶苷的鼻内给药黏膜黏附性给药系统的性能。
采用离子凝胶法制备载有七叶苷的壳聚糖-秋葵胶基纳米粒。以秋葵胶浓度、壳聚糖浓度、pH值和搅拌速度为自变量，粒径、包封率和制剂的zeta电位为因变量，采用Box-Behnken实验设计对制备方法进行优化。用傅里叶变换红外光谱（FTIR）、扫描电子显微镜（SEM）和透射电子显微镜（TEM）对优化后的制剂进行表征。对纳米粒的生物黏附强度和体外药物释放进行研究。将优化后的鼻内制剂给予大鼠，进行药代动力学和生物分布研究，以计算制剂在脑内的靶向效率。
纳米粒的粒径在294.0至613.4nm范围内。发现胶的浓度对粒径和包封率有显著影响。纳米粒的生物黏附强度为32±2%。体外药物释放研究表明，4小时内七叶苷从纳米粒中的释放率为96.4±4.2%。发现纳米粒对脑的药物靶向性几乎是简单溶液形式给予的七叶苷的两倍。
使用壳聚糖-秋葵胶制备的纳米粒具有良好的黏膜黏附强度和较高的脑靶向效率。
